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Protac Services

We have expertise in PROTAC services and synthesis for targeted protein degradation and integrated drug discovery

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PROTACs

(PROteolysis TArgeting Chimeras)

PROTACs are a specific type of molecule or compound designed for targeted protein degradation (TPD). TPD involves employing heterobifunctional small molecules known as "Degraders," like PROTAC Degraders, or utilising PROTAC services to effectively reduce the levels of specific target proteins within cells. PROTACs are heterobifunctional small molecules consisting of a target binding handle bridged via a chemical linker to an E3 ligase handle which hijacks the endogenous ubiquitin machinery to target proteins, resulting in subsequent ubiquitination and degradation of your target of interest.

PROTACs provide significant therapeutic potential with possible prolonged pharmacodynamics, improved potency, and ability to target proteins previously thought of as “undruggable”.

o2h discovery offeres intigrated PROTAC services as well as a bespoke and customisable "off-the-shelf" PROTAC toolbox to jump-start your targeted protein degradation program, along with our strong expertise in medicinal and synthetic chemistry.

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PROTAC services and process

o2h discovery’s expertise in PROTAC services and targeted protein degradation:

In the last few years, we have developed strong expertise in PROTAC services, synthesis and screening of complex PROTAC molecules, and related specialty chemistry. We provide comprehensive solutions for the design and synthesis of PROTAC building blocks, linkers, compound libraries, and related intermediates to help proof and de-risk your targeted protein degradation approach.Read More

We also developed a range of biology capability along with analytical methods and purification protocols for the isolation of high-quality complex PROTAC molecules and their accurate characterisation. Several building blocks have been prepared at gm scale with reliable synthetic routes and purification methodologies.

o2h discovery can provide you a range of E3 ligase ligands from our o2h PROTAC toolboxTM for the quick synthesis of PROTAC equipped with a variety of linkers for rapid assembly of degrader analogues to accelerate your drug discovery and development process with our PROTAC services.Read Less

Listen to what our client says about our protac services

- Julian Blagg, Executive VP, Drug Discovery
- Martin Drysdale, Chief Scientific Officer

o2h PROTAC toolbox™

we offer PROTAC services with our customizable PROTAC toolbox™ kit of over 100 monomers, including various linkers, ligands and necessary controls. They can provide significant therapeutic potential with possible prolonged pharmacodynamics, improved potency, and ability to target proteins previously thought of as “undruggable”.

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protein degradation - biology

biology evaluation suite to estimate ternary complex formation and targeted protein degradation

o2h biologists can support you in addressing the following questions:

Q.Is my target degraded?

Q.Is my target ubiquitinated?

Q.Do they form a ternary complex?

Q.Are they soluble and cell permeable?

Q.What is the binary affinity for POI and E3 ligase?

Q.What is the phenotypic consequence of target degradation?

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case study

PROTAC induced ternary complex formation and kinetics of targeted protein degradation

PROTAC-induced BRD4-VHL ternary complex formation and BRD4 protein degradation. HEK292 cells transfected with NanoLuc-BRD4 donor plasmid and Halo-Tag-VHL acceptor plasmid at 1:100 ratio. Subsequently cells treated with 1uM MZ1 or AT1 PROTAC and compared with untreated DMSO control.

(A, B) Indicates ternary complex formation at 6h (C,D) BRD4-BD2 protein levels at 6h (E,F) real-time ternary complex formation with BRD4-B2/VHL following PROTAC treatment (G,H) real-time kinetics of BRD4-BD2 protein degradation following PROTAC treatment. MG132, a potent, reversible and cell permeable proteasomal inhibitor rescues BRD4 degradation in all condition.

PROTACs purification - analytical capabilities

o2h discovery has analytical capabilities in purification of PROTACs molecules for targeted protein degradation and PROTAC services

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Purification of multiple PROTAC compounds containing various Linkers/Ligands like VHL or CRBN.
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5 years of hands-on experience on PROTAC compounds purification, Available different column chemistry for the purification of PROTAC molecules.
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Successfully enriched the purity level from ~20% to >95%
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Well experienced Analytical team to handle purification from mg to g scale.
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Attained up to 60% practical recovery from prep purification.
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Have effectively purified no. of PROTAC compounds via Prep. HPLC at various scales (mg/g).

case study - VHL ligand chemistry

  • Purified the mentioned PROTAC-molecule by reversed phase Prep. HPLC using basic modifier(pH~9) in water and acetonitrile with gradient elution and the column chemistry used was C18.
  • Collected pure fractions were concentrated using lyophilisation.
  • Crude Quantity was ~1.1 gm with 30% purity of desired product.
  • Successfully isolated ~100 mg in pure form (with 30% recovery)
  • After purification - 95% purity achieved.
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about o2h discovery

o2h discovery has an integrated drug discovery platform operating from its state-of-the-art research centres in Ahmedabad, India, and The Mill Scitech Park, Cambridge, UK.

o2h discovery is a highly reputed service provider of mg/g scale discovery chemistry. We have partnered with a range of well-known pharmaceutical and biotechnology companies from Europe, the USA, and Japan.

our services

A premier Contract Research Organisation providing integrated and biology services for collaborative research

Meet our team

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Sunil Shah

Co-founder, o2h group

Sunil Shah

Sunil Shah

Co-founder, o2h group

A serial entrepreneur having begun a career in the Life Sciences team at PA Consulting group followed by co-founding two companies in the information technology and life sciences sector. The second of these companies, Oxygen Healthcare Ltd was acquired by Piramal Enterprises Ltd (BSE: PEL). Sunil is the Chairman of Exonate and a board member of Cambridge Angels, Biotech Industry Association, and advisory board of the DBT & CRUK affordable cancer medicines initiative. Sunil has a degree in Biochemistry from Keele and an MBA from Cambridge University.

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Prashant Shah

Co-CEO and Co-Founder, o2h group

Prashant Shah

Prashant Shah

Co-CEO and Co-Founder, o2h group

A serial entrepreneur having begun a career with the Strategy group of at Accenture followed by co-founding two companies in the technology and life sciences sector. The second of these companies focused on drug discovery was acquired by a public company. Prashant co-founded o2h Ventures which is involved in seeding, incubating and investing in early stage life science and technology companies. Prashant has a BEng, MSc and an MPhil in Management.

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Andy Morley

Chief Scientific Officer, o2h discovery

Andy Morley

Andy Morley

Chief Scientific Officer, o2h discovery

Creative and innovative medicinal chemist with extensive knowledge and expertise. Twenty five years experience working in the pharmaceutical industry.

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Tejas Upadhyay

VP, Business Development, o2h group

Tejas Upadhyay

Tejas Upadhyay

VP, Business Development, o2h group

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Gayathri Sadasivam

VP, Head of Biology, o2h discovery

Gayathri Sadasivam

Gayathri Sadasivam

VP, Head of Biology, o2h discovery

Gayathri leads the biology capabilities in Ahmedabad, India and Cambridge, UK. She also significantly contributes to the business development with the o2h customers world-wide, understanding the market requirements, contributing to technology transfer and investment evaluations. Prior to this, she has worked for >15 years in different therapeutic areas in both industry and academia. She has led multiple programs in drug discovery projects through lead optimization to candidate selection and further development to late stage clinical trials. She has worked in a multi-disciplinary environment, leading chemical biology efforts creating chemical tools that modulate novel class of “undruggable” targets. Gayathri has a Ph.D. in Neuroscience from the Brain Research Institute, Zurich, Switzerland.

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Claudio Dagostin

VP, Business Development, o2h discovery

Claudio Dagostin

Claudio Dagostin

VP, Business Development, o2h discovery

Claudio got his PhD in Chemistry (Mechanisms of Organic Reactions) from the University in 2000. He went for a post-doc at Imperial College London where he worked on Alzheimer's disease chemical probes. In 2004, he started working in several companies in the Cambridge biotech cluster where he deepened his knowledge in Medicinal Chemistry and in Fragment Based Drug Design. In 2012 he went back to academia at Cambridge University where he investigated challenging drug targets such as protein-protein interactions. He also co-founded the Entrepreneurial Postdocs of Cambridge (EPOC) society in 2015 to support postdocs in their pursuit of entrepreneurial careers. In 2017 joined Capital Cell and then Abzena in Cambridge with a role in Business Development.

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Hemal Soni

Head of Chemistry, o2h discovery

Hemal Soni

Hemal Soni

Head of Chemistry, o2h discovery

Comprehensive experience in Leading & Guiding Multi-FTE “Synthetic Chemistry Research” Collaborations which are in support to fast paced Medicinal Chemistry Projects – for overseas collaborators.

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Dharmesh Bhatt

Analytical Head, o2h discovery

Dharmesh Bhatt

Dharmesh Bhatt

Analytical Head, o2h discovery

Dharmesh obtained his Master’s degree in Chemistry from M.K University and has done MBA in industrial Management from National Institute of Management. He has about 27 years of industrial experience during which he has served many MNCs like Zydus Cadila, Piramal, Dishman Pharma, Daicel etc. He was associated with O2h in 2006 and worked for 3 years and moved to another organization. He re-joined the o2h family back in April-2023. During his professional tenure, Dharmesh has led the Analytical team which includes chromatography and spectroscopy group. He has immense expertise in the purification, isolation & characterization of heterocyclic, macrocyclic, natural products, etc. Dharmesh was also in role of Sales & BD for analytical services, pharma impurity standard, separation services & column business for domestic market. He has been for several years leading a big team of Analytical chemists (currently ~80) who skilfully operate instruments like LCMS, HPLC, SFC, NMR, and Preparative HPLC under his guidance.

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